PREPARATION AND EVALUATION OF COMPRESSION-COATED TABLETS FOR CHRONOPHARMACEUTICAL DRUG DELIVERY

Abstract

Objective: This study aims to prepare and evaluate time-controlled drug delivery system of telmisartan. Telmisartan has low aqueous solubility, which is its major drawback. The solubility of the drug enhanced by using solid dispersion method and compression coated chronotherapeutic tablets were formulated. Material and Method: Solid dispersion of telmisartan was prepared by melting method. Direct compression method was used to prepare telmisartan containing core tablets and tablets were coated by compression-coating method. Prepared tablets were characterized in terms of hardness, diameter, and thickness. In order to demonstrate the pulsatile release, the tablets were subjected to USP Apparatus II dissolution test. Result and Discussion: Solid dispersion of telmisartan increased the solubility of telmisartan significantly (p<0.05). Compression-coated tablets were obtained with suitable hardness values (149.833±5.862-205.367±3.955 N) and telmisartan was released with lag times of 120-540 min which are suitable for chronopharmaceutic application.

Keywords

• Chronopharmaceutical
• compression-coated
• pulsatile release
• solid dispersions
• telmisartan

KRONOFARMASÖTİK İLAÇ TAŞIYICI BASINÇLA KAPLANMIŞ TABLETLERİN HAZIRLANMASI VE DEĞERLENDİRİLMESİ

Abstract

Amaç: Bu çalışmada telmisartanın çözünürlüğünün artırılması için katı dispersiyonlarının hazırlanması amaçlanmıştır. Telmisartanın en önemli sorunu olan düşük çözünürlüğe sahip olmasıdır. Telmisartanın çözünürlüğü katı dispersiyon yöntemi kullanılarak artırılmış ve basınçla kaplanmış kronoterapötik tabletler formüle edilmiştir. Gereç ve Yöntem: Telmisartanın katı dispersiyonları eritme yöntemi ile hazırlanmıştır. Telmisartan katı dispersiyonlarını içeren çekirdek tabletler doğrudan basım yöntemi ile hazırlanmış ve basınçla kaplama yöntemi ile kaplanmıştır. Hazırlanan tabletler sertlik, çap ve kalınlık açısından karakterize edilmiştir. Tabletlerde pulsatil ilaç salımını göstermek amacıyla USP aparat II çözünme hızı testi yapılmıştır. Sonuç ve Tartışma: Telmisartan katı dispersiyonları telmisartanın çözünürlüğünü önemli ölçüde artırmıştır (p<0,05). Basınçla kaplanmış tabletler uygun sertlik değerleri (149,833±5,862-205,367±3,955 N) ve elde edilmiştir. Telmisartan, kronofarmasötik uygulamalara uygun şekilde 120-540 dk arasında değişen gecikme sürelerinden sonra hızla salınmıştır.

Keywords

• Basınçla kaplama
• katı dispersiyon
• kronofarmasötik
• pulsatil salım
• telmisartan

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